EP3946262A1 - Loaded granules, their process of production and their uses - Google Patents

Loaded granules, their process of production and their uses

Info

Publication number
EP3946262A1
EP3946262A1 EP20764081.4A EP20764081A EP3946262A1 EP 3946262 A1 EP3946262 A1 EP 3946262A1 EP 20764081 A EP20764081 A EP 20764081A EP 3946262 A1 EP3946262 A1 EP 3946262A1
Authority
EP
European Patent Office
Prior art keywords
cannabinoid
granules
nicotine
loaded
sugar
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP20764081.4A
Other languages
German (de)
English (en)
French (fr)
Inventor
Xavier SUID
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Evie Sa
Original Assignee
Sakso
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sakso filed Critical Sakso
Priority to EP24158929.0A priority Critical patent/EP4349182A2/en
Publication of EP3946262A1 publication Critical patent/EP3946262A1/en
Pending legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/465—Nicotine; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals

Definitions

  • the present invention concerns orally-dispersible granules containing one or more active cannabinoid compounds, orally-dispersible granules containing nicotine, a process for producing said granules and uses of said granules as nutritional complements.
  • the present invention also relates to said granules for their use as a medicament.
  • the plant Cannabis Sativa L. also called marijuana
  • THC tetrahydrocannabinol
  • CBD cannabidiol
  • CBN cannabinol
  • CBD cannabigerol
  • CBC cannabichromene
  • CBDND cannabinodiol
  • cannabinoid The most notable cannabinoid is the trans-delta9-tetrahydrocannabinol (A9-THC), a powerful psychoactive compound that is responsible of euphoric and mind-altering effects.
  • cannabidiol CBD
  • CBD cannabidiol
  • cannabidiol administration has positive effects to alleviate neuropathic pain in individuals suffering from multiple sclerosis, and in cases of psychosis, movement disorders and anxiety behavorials, including generalized anxiety disorder (GAD), panic disorder (PD), post-traumatic stress disorder (PTSD), social anxiety disorder (SAD) and obsessive-compulsive disorder (OCD).
  • GAD generalized anxiety disorder
  • PD panic disorder
  • PTSD post-traumatic stress disorder
  • SAD social anxiety disorder
  • OCD obsessive-compulsive disorder
  • Cannabidiol administration is well tolerated in humans, across a wide range dose, up to 1500 mg/day (orally), with no reported psychomotor slowing, negative mood effects, or vital sign abnormalities noted (Bergamaschi et al., 2011).
  • Epidiolex® a liquid formulation of highly purified plant-derived cannabidiol, intended for the treatment of two rare, serious childhood epilepsy syndromes.
  • the drug Sativex® comprising CBD and A9-THC in a 1 :1 proportion is approved for the treatment of spasticity due to multiple sclerosis, in numerous countries.
  • This drug is proposed under the form of an oromucosal spray.
  • Isolated phytocannabinoids may be consumed by ingestion, by inhalation or by transdermal delivery.
  • Phytocannabinoids can be extracted from the plant with alcohols, and then applied in the oral cavity. They can also be extracted into oils and then administered orally, or via the nasal mucosa. Oily preparations may be proposed as such, or in the form of sprays, contained in gelatin capsules, or included in transdermal compositions.
  • the patent application WO 2017/189375 discloses chewing gum compositions comprising at least one isolated cannabinoid, nicotine, and at least one flavouring agent and one sweetening agent;
  • nasal cannabidiol compositions comprising an oily vehicle such as a vegetable oil;
  • the patent application WO 2017/180707 relates to ingestible films comprising substances extracted from Cannabis Sativa, said films consisting of a matrix and an isolated cannabinoid in a concentration greater than 90%;
  • the patent application WO 2017/185038 discloses CBD oral formulations comprising furthermore a compound intended for obtaining a fast-acting physiological effect of CBD;
  • the patent application WO 2018/129097 relates to nutritional complements comprising synthetic cannabinoids in combination with N-acetylated fatty amino acids, which increase the water-solubility of cannabinoids;
  • the patent US 10,434,084 describes a powder enriched in cannabinoids, made of tiny coated particles of sugars. This powder may be used as a dry premix for making a beverage or a cooked food;
  • Oily formulations are likely to spill from their vials, and therefore their transport is complicated; moreover, this administration form lacks proper dosage control.
  • the oral formulation allows an easy control of the desired dosage
  • the oral formulation is pleasant to use
  • the oral formulation does not generate any bad taste in the mouth, it does not dry the buccal mucosa;
  • the oral formulation does not need water for its administration; more generally, it does not necessitate any preparation, and can be administrated as it is, under any circumstance (for example while travelling).
  • this oral formulation is also suitable for administering nicotine; the same advantages than those described above are reached for nicotine loaded granules.
  • the oral formulation advantageously comprises at least one terpene.
  • the oral formulation according to the present invention is elegantly presented; its administration is pleasant; in consequence, this formulation is consumed in an enjoyable and playful manner. Furthermore, the consumption of this oral formulation is discreet.
  • the present invention relates to cannabinoid loaded granules consisting of orodispersible sugar granules containing at least one cannabinoid compound.
  • the present invention also relates to nicotine loaded granules consisting of orodispersible sugar granules containing nicotine.
  • the present invention also relates to cannabinoid and nicotine loaded granules consisting of orodispersible sugar granules containing at least one cannabinoid compound and nicotine.
  • said granules are composed of lactose, saccharose, xylitol, or a mix thereof.
  • said cannabinoid and/or nicotine loaded granules further contain at least one terpene, preferably a combination of at least two terpenes.
  • the present invention relates to a process of production of cannabinoid and/or nicotine loaded granules such as described above, comprising at least the following steps: a) Addition to orodispersible sugar granules of at least one cannabinoid compound, and/or of nicotine, b) Air-drying of the granules, c) Repeating of said successive steps (a) and (b) at least twenty times, d) Optionally, coating of the cannabinoid and/or nicotine loaded granules with: a sugar syrup comprising a coloring or a flavoring agent, natural gum, natural wax, or any combination thereof.
  • the present invention also relates to said cannabinoid and/or nicotine loaded granules for their use as a medicament.
  • the present invention also relates to said cannabinoid and/or nicotine loaded granules for their use in the treatment and/or prevention of chronic pain, inflammatory disorders, behavioral disorders, and anxiety disorders.
  • the present invention relates to the use of cannabinoid and/or nicotine loaded granules as a nutritional complement.
  • the present invention also concerns a kit for its use as a nutritional complement, comprising, in a single package, at least two dispensing devices comprising cannabinoid loaded granules further containing at least one terpene, wherein the at least two dispensing devices are distinct from each other in that said at least one terpene is different from one dispensing device to another.
  • cannabinoid compound and “cannabinoid” are used interchangeably and both designate a class of diverse chemical compounds that acts on cannabinoid receptors in cells.
  • This class includes the endocannabinoids (produced naturally in the body by animals), the phytocannabinoids (found in cannabis and some other plants), and synthetic cannabinoids (manufactured artificially).
  • cannabinoid includes all derived forms of cannabinoids, in particular those chemically derived from phyotocannabinoids.
  • THC tetrahydrocannabinol
  • abbreviations A9-THC and THC are used indifferently, both designating trans-A9-tetrahydrocannabinol.
  • Cannabidiol designates the compound referenced under CAS number 13956-29-1, presenting the following developed chemical structure:
  • Cannabidiol has a broad pharmacological profile, including interactions with several receptors, specifically the cannabinoid type 1 receptor (CB1R), the serotonin 5-HT1A receptor, and the transient receptor potential (TRP) vanilloid type 1 (TRPV1 ) receptor.
  • CBD may also regulate, directly or indirectly, the peroxisome proliferator- activated receptor-g, the orphan G-protein-coupled receptor 55, the equilibrative nucleoside transporter, the adenosine transporter, additional TRP channels, and glycine receptors.
  • Cannabidiol has very low affinity for the cannabinoid CBi and CB2 receptors but is said to act as an indirect antagonist of these receptors.
  • Synthetic cannabinoids encompass all chemically synthetized compounds structurally related to THC and cannabidiol, as well as the nonclassical cannabinoids designated as cannabimimetics.
  • Nicotine also designated as 3 - ( N - methyl - 2 - pyr ro lidi ny l ) pyridi ne , 1-methyl-2-(3- pyridyl)pyrrolidine, or b - pyri dy l -a - N - methy Ipy rro li di ne , of CAS number 54-11-5, is a nervous stimulant naturally produced in some plants, in particular tobacco.
  • Nicotine acts as a receptor agonist or antagonist to nicotinic acetylcholine receptors (nAChRs) present in the human brain. After binding to these receptors, nicotine elicits its psychoactive effects and increases the levels of several neurotransmitters in various brain structures.
  • nAChRs nicotinic acetylcholine receptors
  • the present invention concerns cannabinoid and/or nicotine loaded granules consisting of orodispersible sugar granules loaded with at least one cannabinoid compound and/or nicotine.
  • the present invention concerns cannabinoid loaded granules consisting of orodispersible sugar granules loaded with at least one cannabinoid compound.
  • cannabinoid loaded granules designate granules that have been loaded, by any technique known by the person skilled in the art, with at least one cannabinoid compound. Said loading techniques include:
  • the present invention concerns nicotine loaded granules consisting of orodispersible sugar granules loaded with nicotine.
  • the phrase “nicotine loaded granules” designate granules that have been loaded, by any technique known by the person skilled in the art, with nicotine or any one of its derivatives presenting the same psychotropic properties.
  • the present invention concerns cannabinoid and nicotine loaded granules consisting of orodispersible sugar granules loaded with at least one cannabinoid and nicotine.
  • the cannabinoid and/or nicotine loaded granules of the present invention are granules containing cannabinoid(s) and/or nicotine, whatever the loading technique.
  • the term “contain” as used herein to refer to the granules encompasses both the “load into” and “load onto” embodiments.
  • the phrase “cannabinoid and/or nicotine loaded granules” designate granules that have been loaded, by any technique known by the person skilled in the art, with:
  • At least one cannabinoid or (ii) nicotine or any one of its derivatives presenting the same psychotropic properties, or (iii) at least one cannabidiol and nicotine.
  • the orodispersible sugar granules also called pellets or beads, are generally used as homeopathic medicine supports.
  • Homeopathic pills are indeed made from granules made of an inert substance such as sugars, upon which a drop of liquid homeopathic preparation is placed and allowed to evaporate.
  • Neutral orodispersible sugar granules are commercially available and well known by the person skilled in the art.
  • the phrase “neutral granules” designate granules before any step of loading.
  • said o redispersible sugar neutral granules are composed of lactose, saccharose, xylitol, or a mix thereof.
  • the neutral granules are composed of 100% xylitol, a sugar alcohol of CAS number 87-99-0.
  • Xylitol is industrially prepared from lignocellulose, issued from wood and agricultural waste.
  • These granules are orally dispersible (also defined as orodispersible, mouth dissolvable, melt-in-mouth or porous granules), which means that the granules are designed to get dispersed or to disintegrate when they contact saliva, without the aid of water, and then release the active compound (s) they contain. These granules are intended for a sublingual administration of the active compounds they contain.
  • the best time for an orodispersible granule to disintegrate into the mouth is considered to be less than a minute. Usually, the disintegration time varies from 5 to 30 seconds.
  • Neutral granules used for producing cannabinoid loaded granules have preferably a circular shape, such as small beads or balls or spheres.
  • neutral granules and loaded granules of the invention have a diameter superior to 1 millimeter.
  • the diameter of each neutral granule is of about 2 to 10 millimeters, preferably of about 3 to 4 millimeters.
  • each granule presents a diameter of about 3 to 4 millimeters, in particular a diameter of 3.7 millimeters.
  • each neutral granule weights about 30 to 300 milligrams, preferably about 30 to 150 milligrams.
  • these neutral granules are commercially available under batches of “8 for one gram” (i.e. each granule weights about 125 mg), “10 for one gram” (each granule weights about 100 mg), “20 for one gram” (each granule weights about 50 mg), and “25 for one gram” (each granule weights about 40 mg).
  • the cannabinoid that is used for loading neutral granules is selected from the group consisting of: cannabidiol (CBD), cannabigerol (CBG), trans-A9-tetrahydrocannabidiol (THC), and a mix thereof.
  • CBD cannabidiol
  • CBD cannabigerol
  • THC trans-A9-tetrahydrocannabidiol
  • the granules contain cannabidiol (CBD). These granules are especially intended for individuals wishing to consume only cannabidiol, via a sublingual way of administration.
  • the granules contain a product such as PURE CBD, an isolate of cannabidiol.
  • the granules contain trans-A9-tetrahydrocannabidiol (THC).
  • the granules contain a mix of both cannabidiol (CBD) and trans-A9-tetrahydrocannabidiol (THC).
  • CBD cannabidiol
  • THC trans-A9-tetrahydrocannabidiol
  • CBD and THC can be combined in a specific ratio, comprised between 99:1 of CBD/THC and 1 :99 of CBD/THC, the limit values of this range being included.
  • CBD and THC have many overlapping physiological effects, although they work via different mechanisms of action. When combined, CBD and THC can enhance each other’s benefits while reducing unwanted effects, including the psychoactive or impairing effects of THC.
  • the granules contain cannabidiol (CBD), trans-A9- tetrahydrocannabidiol (THC), or a mix thereof, and a further other cannabinoid compound.
  • CBD cannabidiol
  • THC trans-A9- tetrahydrocannabidiol
  • the granules contain cannabidiol (CBD) in combination with cannabigerol (CBG).
  • CBD cannabidiol
  • CBG cannabigerol
  • the at least one cannabinoid used for loading the neutral granules may be of natural origin or synthetic.
  • the at least one cannabinoid is a phytocannabinoid of natural origin.
  • the at least one cannabinoid may be a phytocannabinoid extracted from the plant Cannabis sativa.
  • the at least one cannabinoid will be under a purified form comprising at least
  • This purified form might be in particular an isolate of said cannabinoid.
  • Extracts from the plant Cannabis sativa might be under different forms such as emulsion, oil, paste, liquid, resin, crystal, powder, or pulp. These different forms of cannabinoid extract are classified in two main categories: “full spectrum” or “isolate”.
  • the “full spectrum” contains mainly one cannabinoid, but also small amounts of other cannabinoids from the plant.
  • the “isolate” consists of the purified cannabinoid that has been extracted from the plant and isolated from the other cannabinoids.
  • said isolate contains at least 95%, preferably at least 99% and more preferably about 99.9% in weight of the considered cannabinoid, compared to the total weight of the isolate.
  • Cannabidiol isolates with more than 99% of CBD are commercially available, for example at SPECTRUMS Europe or at FOLIUM BIOSCIENCES (US).
  • the granules are sugar coated with a sugar syrup and an extract containing at least one cannabinoid compound and/or nicotine.
  • Coating turbines useful for this step are in particular those of type DRIAM, GLATT or MANESTY.
  • the process of sugar coating comprises three steps: coating of the granules with a sugar syrup, then application onto the granules of an extract containing at least one cannabinoid compound (full-spectrum or isolate, preferentially an isolate), and/or nicotine, and finally air-drying of the coated granules.
  • the sugar syrup consists of water and at least one sugar, such as a polyol, a monosaccharide, a disaccharide, or any combination thereof.
  • the sugars are chosen among lactose, saccharose, a polyol or a mix thereof.
  • the sugar is a polyol, and preferably is xylitol.
  • the sugar syrup is in a concentration of about “60 BRIX”, corresponding to 60 grams of sugar dissolved in 100 ml of water.
  • the sugar syrup might also be a solution at 40, 50, 65, 70, 80 or 90 BRIX.
  • the extract containing at least one cannabinoid compound is derived from the plant Cannabis Sativa L.
  • it is an isolate comprising only one cannabinoid compound.
  • this isolate comprises at least 95% by weight of said one cannabinoid compound.
  • Dose of the loaded cannabinoid Dosage is the key factor in achieving the most benefits and least adverse effects of Cannabis sativa extracts. Although variable from one individual to another, optimal (i.e. safe, with no side effects) mean day doses of cannabinoid for adults have been established by physicians, and are the following:
  • CBD 25 to 30 milligrams per day
  • THC 20 to 30 milligrams per day.
  • each single dose of administration shall not exceed 10 mg.
  • the cannabinoid loaded granules are prepared to contain a specific amount of at least one cannabinoid or a mix thereof.
  • each granule may contain 5, 10, 15, 20, 25 or 30 mg of cannabinoids, i.e. of one single cannabinoid or of a mix of at least two cannabinoid compounds.
  • each granule contains a dose of one cannabinoid from about 2 mg to about 8 mg, preferentially from about 4 mg to about 6 mg, and more preferably a dose equal to about 5 mg.
  • the at least one cannabinoid represents 3.85 % of the total dry weight of the loaded granule.
  • the at least one cannabinoid represents 11.11 % of the total dry weight of the loaded granule.
  • the at least one cannabinoid represents about 2 % to 15% in weight of the total dry weight of the cannabinoid loaded granule. Dose of loaded nicotine
  • Dosage is the key factor in achieving the most benefits and least adverse effects of nicotine. Although variable from one individual to another, physicians have established that for smoking suspension or cessation, about 1 mg of nicotine shall be administered for each daily consumed cigarette by the individual.
  • each single dose of administration shall not exceed 30 mg of nicotine.
  • the nicotine loaded granules are prepared to contain a specific amount of nicotine.
  • each granule may contain 5, 10, 15, 20, 25 or 30 mg of nicotine.
  • the invention relates to: loaded granules contain cannabidiol (CBD) in combination with nicotine; loaded granules contain trans-A9-tetrahydrocannabidiol (THC) in combination with nicotine; loaded granules contain a mix of both cannabidiol (CBD) and trans-A9- tetrahydrocannabidiol (THC) and nicotine; loaded granules contain cannabidiol (CBD) in combination with cannabigerol (CBG) and nicotine.
  • CBD cannabidiol
  • CBG cannabigerol
  • the cannabinoid and/or nicotine loaded granules further contain at least one terpene, preferably a combination of at least two terpenes.
  • the invention concerns: cannabinoid loaded granules further containing at least one terpene, preferably a combination of at least two terpenes; - nicotine loaded granules further containing at least one terpene, preferably a combination of at least two terpenes; and cannabinoid and nicotine loaded granules further containing at least one terpene, preferably a combination of at least two terpenes.
  • the cannabinoid and/or nicotine loaded granules of the invention are impregnated with a solution comprising a combination of at least two terpenes.
  • Terpenes are a class of organic hydrocarbons that are produced by a variety of plants, particularly conifers, and by some insects. Terpenes and their derivative terpenoids are the primary constituents of the essential oils. Terpenes are also major constituents of Cannabis sativa plants, which contain at least 120 identified compounds. Terpenes have desirable properties for use in food and pharmaceutical industries. While terpenes and terpenoids occur widely, their extraction from natural sources is often problematic. Consequently, they are often supplied as synthetic products issued from chemical synthesis.
  • the granules are impregnated with a solution comprising at least one terpene chosen among the following group: myrcene, d-limonene, alpha-pinene, linalol, borneol, carophyllene, terpinolene, menthol, geraniol, bisabolol, beta-caryophyllene, humulene, linalool, farnesene, a-phellandrene, and any combination thereof.
  • Impregnation of granules is a routine procedure for the person skilled in the art of homeopathic granules. The procedure has been extensively described in literature, for example in US patent 4,703,717. This technique comprises the use of: a liquid comprising the active compounds (at least one terpene), porous sugar granules of a desired size/weight; and - an impregnating device, with control means.
  • Impregnating devices are commercially available, in any homeopathic devices shop, such as for example at http://www.vanda-france.fr/.
  • the granules of the invention are impregnated with terpene(s) at a rate of 0.2 % to 2 %, preferably at a rate of impregnation of 0.5 %.
  • a common dose is about 25 grams of terpenes for 5000 grams of xylitol granules, corresponding to an impregnation rate of 0.5%.
  • the granules are firstly impregnated with a dynamized solution comprising at least one terpene, and then are loaded with cannabinoid(s) and/or nicotine.
  • loaded granules can be coated with a natural gum, for example with arabic gum, right after the step of terpenes impregnation. This optional step is useful to fix and isolate the at least one terpene, and further helps to solidify the granule.
  • Cannabinoid and/or nicotine loaded granules according to the invention may also comprise at least one additional active compound.
  • Mushroom extracts are in particular extracts from the following mushrooms:
  • Hydnum repandum commonly known as the sweet tooth, wood hedgehog or hedgehog mushroom, a Basidiomycete fungus of the family Hydnaceae;
  • Hericium erinaceus also called lion's mane mushroom, monkey head mushroom, bearded tooth mushroom, satyr's beard, bearded hedgehog mushroom, pom pom mushroom, or bearded tooth fungus, belonging to the tooth fungus group; chaga, i.e. Inonotus obliquus, from the family Hymenochaetaceae ; reishi, also known as Lingzhi or Ganoderma lingzhi, a polypore fungus belonging to the genus Ganoderma;
  • Trametes versicolor also known as Coriolus versicolor or Polyporus versicolor, a polypore mushroom.
  • cannabinoid and/or nicotine loaded granules according to the invention further comprise at least one mushroom extract.
  • cannabinoid and/or nicotine loaded granules according to the invention further comprise caffeine.
  • cannabinoid and/or nicotine loaded granules according to the invention further comprise at least one flavonoid.
  • the cannabinoid and/or nicotine loaded granules may further contain additional compounds selected from the group of solubilizers, thickeners, surfactants, coloring agents (in particular for whitening the granules), flavoring agents, effervescent agents, antioxidants, bioadhesive agents, pH modifying agents, vitamins, minerals, permeability or penetration enhancers, absorption enhancers, serotonin, caffeine, amino acids, and mixtures thereof. Permeability or penetration enhancers and absorption enhancers, if present, are added in order to improve the absorption of the cannabinoid by the mucosal tissues of an individual.
  • Vitamins are in particular selected from the group consisting of thiamin, riboflavin, nicotinic acid, pantothenic acid, pyridoxine, biotin, folic acid, vitamin B12, lipoic acid, ascorbic acid, vitamin A, vitamin D, vitamin E, and vitamin K.
  • additional compounds may be added to the granules by impregnation or as part of the sugar-coating of the granules.
  • Final coating of the cannabinoid and/or nicotine loaded granules enables an aesthetic appeal, while improving the stability of the granules. In particular, if traces of crystalline powder of the cannabinoid isolate are still present around the loaded granules, the final coating might allow the fixation of said powder traces onto the granule.
  • the cannabinoid and/or nicotine loaded granules are coated with: a sugar syrup comprising a coloring or flavoring agent, natural gum, natural wax, or any combination thereof.
  • This optional step allows the obtention of bright granules. Further, this final coating protects them from breakage. The technique for obtaining this coating has been described above.
  • This final coating is an outer layer on the whole surface of the granule, of a thickness inferior to 10 microns. It might comprise notably:
  • a natural gum such as arabic gum or xanthan gum; or A natural wax such as carnauba wax or beeswax; or
  • a sugar coating o A polyol such as xylitol; or o A monosaccharide such as glucose or fructose; or o A di saccharide such as saccharose, lactose, or sucrose, or Any combination thereof.
  • the final coating layer may comprise coloring and/or flavoring agents.
  • the final coating layer may comprise a coloring agent chosen from appropriate synthetic or natural coloring agents, well known by the person skilled in the art.
  • the final coating layer may also contain flavoring agents chosen from synthetic flavor oils and flavoring aromatics and/or natural oils.
  • flavoring agents might be chosen among those having one of the following flavors : mint, ginger, anise, cinnamon, peppermint, licorice, honey, vanilla, citrus oil, including lemon, orange, grape, lime and grapefruit, and fruit essences, including apple, pear, peach, strawberry, raspberry, cherry, plum, pineapple, apricot and so forth.
  • the present invention also concerns a process of production of cannabinoid and/or nicotine loaded granules such as described above, comprising at least the following steps: a) Addition to orodispersible sugar granules of at least one cannabinoid compound, and/or of nicotine, b) Air-drying of the granules, c) Repeating of said successive steps (a) and (b) at least twenty times, d) Optionally, coating of the cannabinoid and/or nicotine loaded granules with: a sugar syrup comprising a coloring or a flavoring agent, natural gum, natural wax, or any combination thereof.
  • the step of “addition to orodispersible sugar granules” can be performed by any technique known by the person skilled in the art. In particular, this step of addition of at least one cannabidiol compound and/or nicotine might be:
  • Optional steps can be added, at any time during the process described above: for example, a step of terpene(s) impregnation, followed by a step of scrubbing, can be implemented before or after the cannabinoid and/or nicotine loading step (a).
  • the process of production of cannabinoid and/or nicotine loaded granules comprises at least the following steps: a1 ) Coating of orodispersible sugar granules with a sugar syrup, in particular a xylitol syrup, a2) Application onto the xylitol -coated granules of an extract containing at least one cannabinoid compound and/or nicotine, b) Air-drying of the granules, c) Repeating of said successive steps (a1), (a2) and (b), at least twenty times, d) Optionally, further coating of the cannabinoid and/or nicotine loaded granules with: a sugar syrup comprising a coloring or a flavoring agent, natural gum, natural wax, or any combination thereof.
  • step (a1) orodispersible sugar granules are sprayed with a sugar syrup such as a xylitol syrup.
  • a sugar syrup such as a xylitol syrup.
  • These granules might have been previously impregnated with a solution comprising at least one terpene, preferably a combination of at least two terpenes.
  • Steps (a1), (a2) and (b) are performed in a coating turbine. These steps are realized successively and are repeated at least twenty times, preferably at least thirty times, more preferably at least forty times, and in a preferred manner about fifty times.
  • Step (d) consists of the final sugar-coating of the cannabinoid and/or nicotine loaded granules, with a thin outer layer on the whole surface of the granule, comprising:
  • a natural gum such as arabic gum or xanthan gum; or A natural wax such as carnauba wax or beeswax; or - A sugar coating comprising water and : o A polyol such as xylitol; or o A monosaccharide such as glucose or fructose; or o A di saccharide such as saccharose, lactose, or sucrose, and o
  • a flavoring agent and/or a coloring agent or - Any combination thereof.
  • This step (d) can be repeated at least twice, for example:
  • a first sugar-coating step is realized in order to cover the granules with a flavoring agent
  • a second coating step is realized with wax, for obtaining a bright appearance of the cannabinoid and/or nicotine loaded granule.
  • the first sugar-coating step for covering the granules with a flavoring agent can be repeated at least twice, at least five times, at least ten, twenty or more times, before performing the second coating step.
  • Coating turbines useful for this step are in particular those of type DRIAM, GLATT or MANESTY.
  • the present invention is also related to a process of production of cannabinoid loaded granules, comprising at least the following steps: a) Lyophilization of a solution comprising at least one cannabinoid compound and one sugar, b) Formation of granules from the lyophilized powder, for example using a tablet press, c) Optionally, coating of the cannabinoid loaded granules with: a sugar syrup comprising a coloring or a flavoring agent, natural gum, natural wax, or any combination thereof.
  • This process is particularly useful in the case of the at least one cannabinoid compound is THC. This process is illustrated in example 5.
  • the present invention also concerns cannabinoid and/or nicotine loaded granules as described above, or as obtained by anyone of the processes as described above, for their use as a medicament.
  • Cannabinoid and/or nicotine loaded granules are intended to be administered sublingually.
  • this delivery route of cannabinoid (s) allows a rapid onset of the cannabinoid(s) through the oral mucosa membranes.
  • the invention concerns said cannabinoid and/or nicotine loaded granules for their use in the treatment and/or prevention of chronic pain, inflammatory disorders, behavioral disorders, and anxiety disorders.
  • treat refers to the administration of therapy to an individual in an attempt to reduce the frequency and/or severity of symptoms of a disease, defect, disorder, or adverse condition of said individual.
  • the terms “prevent”, “preventing” or “prevention” refers to the administration of a therapeutic compound to an individual in an attempt to reduce the likelihood for said individual to develop a specific disease.
  • the invention concerns nicotine loaded granules for their use in the treatment of tobacco addiction, on an occasional or regular basis.
  • Nutritional complement and kit comprising it
  • the present invention also relates to the use of cannabinoid and/or nicotine loaded granules as described above, or as obtained by anyone of the processes as described above, as a nutritional complement.
  • the term “nutritional complement” designates any dietary complement that comes further to the normal dietary regimen that is intended to provide substances that are not usually consumed.
  • the present invention also relates to a kit for its use as a nutritional complement, comprising, in a single package, at least two dispensing devices comprising cannabinoid loaded granules further containing at least one terpene, wherein the at least two dispensing devices are distinct from each other in that said at least one terpene is different from one dispensing device to another.
  • said kit further comprises means for communicating information or instructions for the use of said kit.
  • said kit comprises cannabidiol loaded granules.
  • an optimal daily dose of a cannabinoid such as cannabidiol (CBD)
  • CBD cannabidiol
  • the user of the kit will choose 5 granules to consume during the day, according to his/her specific needs: concentration, sleepiness, fatigue, energy-load before exercising, etc.
  • the user might choose to consume two granules in the morning from one dispensing device, one granule at noon from another dispensing device, and two granules before sleeping at night from the last dispensing device.
  • the kit of the invention comprises enough granules for administration over one week (35 cannabinoid loaded granules), two weeks (70 cannabinoid loaded granules) or even one month (more than 140 cannabinoid loaded granules), the number of granules being based on the optimal daily dose of 5 granules a day.
  • These granules are distributed in at least two dispensing devices, preferably in three, four, five, six or seven dispensing devices.
  • Each dispensing device comprises about 5, 10, 15, 20, 25 or 30 cannabinoid loaded granules.
  • Example 1 Process of preparation of cannabinoid loaded granules
  • xylitol granules have been loaded with 5 mg of CBD per granule.
  • Used xylitol beads are about 3.7 mm in diameter and 0.04 g in weight.
  • a solution comprising a combination of pure terpenes (Myrcene type) such as limonene, A-pinene, linalol, carophyllene, was used in the following proportion:
  • Dynamization of the solution was repeated three times: during 20 seconds, 300 succussions.
  • liquid containing the active components are preferentially “dynamized” before impregnation.
  • dynamization refers to the vigorous shaking of an alcoholic solution comprising an active compound, in a process called "succussion”.
  • Impregnation is realized either with an impregnator or with a coating turbine.
  • xylitol beads are impregnated with a combination of at least two terpenes (in this case, 5 g of terpenes for 1 kg of beads, i.e. 0.5% terpenes by weight per bead).
  • B - Coating of xylitol beads impregnated with terpenes with xylitol syrup and then application of CBD or any other cannabinoid compound In this example, 2 kg of xylitol beads (i.e. about 50000 beads) impregnated with terpenes were used, with 250 g of cannabidiol (CBD), in order to dispense about 5 mg of CBD to each bead.
  • CBD cannabidiol
  • a xylitol syrup at 60 BRIX was prepared with 450 g of xylitol and 300 g of water, heated up to 80° C, then the temperature of the syrup is decreased between 50° C and 60° C, and the concentration of xylitol is adjusted to 60 BRIX.
  • the xylitol beads are introduced into the turbine for the coating.
  • Each cycle of coating and application of CBD comprises the following substeps: Beads are sprayed with xylitol syrup, with an automatic spray gun, and then mixed for about 30 seconds;
  • CBD isolate is applied onto beads
  • Beads are dried with air treatment for 3 to 4 minutes, with a “cold” air at a temperature of about 25 °C. These successive steps are repeated about 64 times.
  • n° 21 16 sprays of xylitol syrup / CBD isolate are performed, during which 4.5 g of cannabidiol are loaded. With this process, the 250 g of cannabidiol are progressively introduced onto the 50 000 beads.
  • Example 2 Further coating of cannabinoid loaded granules for flavour, colour and/or brightness
  • Beads are sprayed with xylitol syrup with an automatic spray gun, and mixed for about 4 minutes;
  • Beads are dried with air treatment, for about 3 minutes; During the last spray, vanilla flavour (2 g/kg) is added to the beads, with minimal air;
  • Carnauba wax is mixed with the CBD loaded granules, without any air, in the following proportion: 500 mg of wax for 1 kg of loaded granules.
  • a kit comprising xylitol granules loaded with 5 mg CBD per granule, and other active compounds comprises eight dispensing devices.
  • Each dispensing device comprises CBD-loaded granules comprising furthermore a mix of terpenes, said dispensing devices being distinct from each other in that said mix of terpenes is different from one dispensing device to another.
  • each granule comprises 0.5% terpenes mix by weight.
  • Each one of the eight dispensing devices is designed for a specific use: 1) BRAIN FOCUS - “FOCUS”
  • CBD-loaded granules comprise furthermore a combination of at least two terpenes chosen among: alpha-pinene, d-limonene, borneol and myrcene.
  • CBD-loaded granules comprise furthermore a combination of of at least two terpenes chosen among: alpha-pinene, d-limonene, terpinolene, menthol, geraniol and bisabolol.
  • CBD-loaded granules comprise furthermore a combination of at least two terpenes chosen among: alpha-pinene, beta-Caryophyllene, Humulene, linalool, and myrcene.
  • CBD-loaded granules comprise furthermore a combination of at least two terpenes chosen among: alpha-pinene, d-limonene, geraniol, humulene, farnesene, linalool and myrcene.
  • SAFEGUARD Immunosystem booster
  • IMMUNITY CBD-loaded granules comprise furthermore a combination of at least two terpenes chosen among: alpha-pinene, d-limonene, beta-caryophyllene, a-phellandrene, linalool and myrcene.
  • APHRODISIAC STIMULANT (sensitive) - “INTIMACY” CBD-loaded granules comprise furthermore a combination of at least two terpenes chosen among: alpha-pinene, d-limonene, terpinolene, beta-caryophyllene, humulene, farnesene, linalool and myrcene.
  • CBD-loaded granules comprise furthermore a combination of at least two terpenes chosen among: farnesene, beta-caryophyllene, myrcene.
  • CBD-loaded granules with a combination of at least two terpenes CBD is said “pure” since these granules do not contain any cannabigerol (CBG).
  • CBD cannabigerol
  • Air temperature between 20° - 30°
  • Granules made of xylitol (5000 g) are deposited into the coating device.
  • the device is turned on.
  • Mixing speed is comprised between 30 and 40 rpm (revolutions per minute).
  • Terpenes and alcohol are mixed with dynamization: 2 to 6 times / between 300 and 500 succussions.
  • the dynamized solution is integrated in 4 steps into the coating device, and then: brewing for 10 to 30 minutes drying for 30 to 60 minutes, at a temperature comprised between 40° and 60° C.
  • Blend xylitol powder and arabic gum Blend xylitol powder and arabic gum.
  • Blend xylitol powder and arabic gum Heat water up to 30° - 45 °C
  • Xylitol powder between 2700g et 3500g
  • Distilled water between 1000g et 1700g CBD - CBG: about 1400g
  • This coating process comprises between 40 et 70 steps. Each step consists of:
  • This coating process comprises between 10 et 30 steps. Each step consists of the following substeps:
  • Example 5 Illustration of another industrial process of preparation of THC loaded granules This process comprises the following steps:
  • the solution is homogenized by dynamization.
  • the final solution is homogenized by ultrasonic homogenization
  • the operation is repeated up to the obtention of particles of a size between 100 and 200 microns.
  • the solution is dispensed into the trays Incubation in the freezer dryer: o 9 to 12 hours of freezing o 24 to 28 hours of lyophilization
  • the lyophilized powder is mixed with an excipient (Mannitol, xylitol.%) in the following proportions: - 43% Lyophilized powder
  • Powder homogenization is carried out by dry granulation, hammer granulator or wheel granulator. Particles of a size between 100 and 200 microns are obtained. 6. Powder shaping
  • Granules of diameter comprised between 3 to 4 mm are formed using the tablet press.
  • the coating process consists of between 10 and 30 steps. Each step consists of the following substeps: o Addition of about 50 ml of Xylitol syrup (69% Xylitol - 31% water) into the coating machine; o Stirring between 1 and 5 minutes; o Drying between 20° and 30° Celsius
  • Granules are refill into the coating machine; Addition of carnauba wax on the granules; Brewing between 30 minutes and 1 hour.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physiology (AREA)
  • Polymers & Plastics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Food Science & Technology (AREA)
  • Mycology (AREA)
  • Botany (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (AREA)
EP20764081.4A 2019-08-30 2020-08-28 Loaded granules, their process of production and their uses Pending EP3946262A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP24158929.0A EP4349182A2 (en) 2019-08-30 2020-08-28 Loaded granules, their process of production and their uses

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19306056 2019-08-30
PCT/EP2020/074062 WO2021038029A1 (en) 2019-08-30 2020-08-28 Loaded granules, their process of production and their uses

Related Child Applications (1)

Application Number Title Priority Date Filing Date
EP24158929.0A Division EP4349182A2 (en) 2019-08-30 2020-08-28 Loaded granules, their process of production and their uses

Publications (1)

Publication Number Publication Date
EP3946262A1 true EP3946262A1 (en) 2022-02-09

Family

ID=68536744

Family Applications (2)

Application Number Title Priority Date Filing Date
EP20764081.4A Pending EP3946262A1 (en) 2019-08-30 2020-08-28 Loaded granules, their process of production and their uses
EP24158929.0A Pending EP4349182A2 (en) 2019-08-30 2020-08-28 Loaded granules, their process of production and their uses

Family Applications After (1)

Application Number Title Priority Date Filing Date
EP24158929.0A Pending EP4349182A2 (en) 2019-08-30 2020-08-28 Loaded granules, their process of production and their uses

Country Status (11)

Country Link
US (1) US20220295853A1 (ja)
EP (2) EP3946262A1 (ja)
JP (1) JP2022547409A (ja)
KR (1) KR20220054331A (ja)
CN (1) CN114828825A (ja)
AU (1) AU2020335245A1 (ja)
BR (1) BR112022003555A2 (ja)
CA (1) CA3151691A1 (ja)
IL (1) IL290914A (ja)
MX (1) MX2022002467A (ja)
WO (1) WO2021038029A1 (ja)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023245107A1 (en) * 2022-06-15 2023-12-21 Phyto Tech Corp. Microencapsulation of cannabidiol or its mixture with nicotine for oral and topical administration

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2574659B1 (fr) 1984-12-19 1987-01-02 Boiron Lab Sa Chaine de fabrication pour des medicaments homeopathiques, notamment pour l'impregnation des granules ou globules
DE10296335T5 (de) 2001-02-14 2004-04-15 G W Pharma Ltd., Salisbury Pharmazeutische Formulierungen
FR2967066B1 (fr) * 2010-11-04 2013-06-14 Ethypharm Sa Utilisation par voie sublinguale de microgranules non comprimes
US9095563B2 (en) 2013-09-26 2015-08-04 Ronald D. Sekura Topical treatments incorporating Cannabis sp. derived botanical drug product
DE102014213548A1 (de) * 2014-07-11 2016-01-14 Hans Brammer Cannabispräparat
CA3020798A1 (en) 2016-04-12 2017-10-19 Scott SCHANEVILLE Ingestible films having substances from hemp or cannabis
KR102393596B1 (ko) 2016-04-22 2022-05-04 리셉터 홀딩스, 인크. 속효성 식물-계 의약 화합물 및 영양 보충제
WO2017189375A1 (en) 2016-04-27 2017-11-02 Axim Biotechnologies, Inc. Chewing gum composition comprising cannabinoids and nicotine
US10653639B2 (en) * 2016-05-16 2020-05-19 Cv Sciences, Inc. Pharmaceutical formulations containing cannabidiol and nicotine for treating smokeless tobacco addiction
TWI790204B (zh) 2016-06-02 2023-01-21 加拿大商阿爾宙斯製藥有限公司 鼻用大麻素組成物
US20190133940A1 (en) * 2016-06-30 2019-05-09 Philip Morris Products S.A. Nicotine particles and compositions
US10434084B2 (en) * 2016-11-29 2019-10-08 Scientific Holdings, Llc Cannabinoid blends and formulations, related methods
KR20190103302A (ko) 2017-01-03 2019-09-04 리셉터 홀딩스, 인크. 의약 화합물 및 영양 보충제
WO2019036243A1 (en) 2017-08-16 2019-02-21 Molecular Infusions, Llc Formulations
US20180344786A1 (en) * 2017-06-06 2018-12-06 NC3 Systems System and method enhanced cannabiniod effect delivery

Also Published As

Publication number Publication date
WO2021038029A1 (en) 2021-03-04
IL290914A (en) 2022-04-01
AU2020335245A1 (en) 2022-03-10
MX2022002467A (es) 2022-05-19
KR20220054331A (ko) 2022-05-02
US20220295853A1 (en) 2022-09-22
JP2022547409A (ja) 2022-11-14
CN114828825A (zh) 2022-07-29
CA3151691A1 (en) 2021-03-04
BR112022003555A2 (pt) 2022-05-24
EP4349182A2 (en) 2024-04-10

Similar Documents

Publication Publication Date Title
US20090155392A1 (en) Methods and Systems for Sublingual Guarana Administration
US20200022905A1 (en) Composition for buccal absorption of nicotine for the purpose of smoking cessation and method for administering
JP2002541123A (ja) オーバーコートしたチューインガム配合物
US10441535B2 (en) Nutraceutical confectionary composition containing caffeine and L-theanine
CN110944632A (zh) 睡眠障碍组合物及其治疗
US20120121520A1 (en) Functional formulation in chewing gum
KR102539374B1 (ko) 뇌 활성 증진용 조성물
WO2021038029A1 (en) Loaded granules, their process of production and their uses
US11752108B2 (en) Gold particles including an oleo-gum resin and/or a derivative thereof and methods of preparing and using the same
WO2013186220A1 (en) Compositions comprising hesperidin and/or apigenin i.a. for medical use or for use in treatment of sleeping disorders
EP1945181B1 (en) Coated pharmaceutical composition for buccal release which comprises a consumable center and a medicament-containing coating
WO2017036488A1 (fr) Produit de combinaison pour aider a la relaxation et a l'endormissement
WO2017109300A1 (fr) Produit de combinaison pour aider à la relaxation et à l'endormissement
KR102245027B1 (ko) 상추 및 황금 추출물을 유효성분으로 함유하는 수면 장애 개선용 조성물
US20050053555A1 (en) Appetite control compositions and methods of use
WO2018108238A1 (fr) Produit de combinaison pour aider à la relaxation et à l'endormissement
JP6698034B2 (ja) 冷え症等の全身症状改善用経口組成物
JP7466748B1 (ja) 肝機能の維持又は改善用組成物
WO2023118485A1 (fr) Combinaison de plantes pour aider a la relaxation et a l endormissement
US20110268717A1 (en) Herbal-Based Compositions for Alleviating Symptoms Associated with Autism
US20210169795A1 (en) Colloidal Suspensions of Plant Extracts in Aqueous Solutions
JP2023504753A (ja) 活性成分の組合せを含む口腔用製品
EP1964551A1 (en) Compositions for the prevention and treatment of primary headache and migraine
US20050053558A1 (en) Sleep inducing toothpaste made with natural herbs and a natural hormone
JP2014122246A (ja) Ｍａｇｎｏｌｉｉｄａｅ化合物を製造する方法

Legal Events

Date Code Title Description
STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: UNKNOWN

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE INTERNATIONAL PUBLICATION HAS BEEN MADE

PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: REQUEST FOR EXAMINATION WAS MADE

17P Request for examination filed

Effective date: 20211028

AK Designated contracting states

Kind code of ref document: A1

Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: EXAMINATION IS IN PROGRESS

DAV Request for validation of the european patent (deleted)
DAX Request for extension of the european patent (deleted)
17Q First examination report despatched

Effective date: 20221128

TPAC Observations filed by third parties

Free format text: ORIGINAL CODE: EPIDOSNTIPA

RAP1 Party data changed (applicant data changed or rights of an application transferred)

Owner name: EVIE SA

P01 Opt-out of the competence of the unified patent court (upc) registered

Effective date: 20230525

GRAP Despatch of communication of intention to grant a patent

Free format text: ORIGINAL CODE: EPIDOSNIGR1

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: GRANT OF PATENT IS INTENDED

RIC1 Information provided on ipc code assigned before grant

Ipc: A23L 33/105 20160101ALI20231115BHEP

Ipc: A61P 29/00 20060101ALI20231115BHEP

Ipc: A61K 9/50 20060101ALI20231115BHEP

Ipc: A61K 9/16 20060101ALI20231115BHEP

Ipc: A61K 9/00 20060101AFI20231115BHEP

INTG Intention to grant announced

Effective date: 20231220

TPAC Observations filed by third parties

Free format text: ORIGINAL CODE: EPIDOSNTIPA

GRAS Grant fee paid

Free format text: ORIGINAL CODE: EPIDOSNIGR3

GRAJ Information related to disapproval of communication of intention to grant by the applicant or resumption of examination proceedings by the epo deleted

Free format text: ORIGINAL CODE: EPIDOSDIGR1

GRAL Information related to payment of fee for publishing/printing deleted

Free format text: ORIGINAL CODE: EPIDOSDIGR3

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: EXAMINATION IS IN PROGRESS

TPAC Observations filed by third parties

Free format text: ORIGINAL CODE: EPIDOSNTIPA

GRAP Despatch of communication of intention to grant a patent

Free format text: ORIGINAL CODE: EPIDOSNIGR1

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: GRANT OF PATENT IS INTENDED

TPAC Observations filed by third parties

Free format text: ORIGINAL CODE: EPIDOSNTIPA

INTC Intention to grant announced (deleted)
GRAS Grant fee paid

Free format text: ORIGINAL CODE: EPIDOSNIGR3

GRAJ Information related to disapproval of communication of intention to grant by the applicant or resumption of examination proceedings by the epo deleted

Free format text: ORIGINAL CODE: EPIDOSDIGR1

GRAL Information related to payment of fee for publishing/printing deleted

Free format text: ORIGINAL CODE: EPIDOSDIGR3

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: EXAMINATION IS IN PROGRESS

INTG Intention to grant announced

Effective date: 20240422